262296-01-5Relevant academic research and scientific papers
ANTIBACTERIAL PICOLINAMIDE COMPOUNDS
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, (2022/01/12)
Here we report the discovery of 2-(4-(3-(trifluoromethoxy)phenoxy)picolinamido) benzo[d]oxazole-5-carboxylate as an antibacterial with potent and selective activity against C. difficile. Its MIC50 andMIC90 values,documented across 101 strains of C. difficile, are 0.12 and 0.25 μg/mL, respectively. The compound is effective against C. difficile both at the logarithmic (vegetative) and stationary phases of growth. It targets cell-wall biosynthesis, as assessed both by macromolecular biosynthesis assays and by scanning-electron microscopy. Animals infected with a lethal dose of C. difficile and treated with compound 1 had better survival compared to treatment with vancomycin, which is the front-line antibiotic used for severe recurrent C. difficile infection.
Structure-Activity Relationship for the Picolinamide Antibacterials that Selectively Target Clostridioides difficile
Speri, Enrico,Qian, Yuanyuan,Janardhanan, Jeshina,Masitas, Cesar,Lastochkin, Elena,De Benedetti, Stefania,Wang, Man,Schroeder, Valerie A.,Wolter, William R.,Oliver, Allen G.,Fisher, Jed F.,Mobashery, Shahriar,Chang, Mayland
, p. 991 - 995 (2021/05/27)
Clostridioides difficile is a leading health threat. This pathogen initiates intestinal infections during gut microbiota dysbiosis caused by oral administration of antibiotics. C. difficile is difficult to eradicate due to its ability to form spores, which are not susceptible to antibiotics. To address the urgent need for treating recurrent C. difficile infection, antibiotics that selectively target C. difficile over common gut microbiota are needed. We herein describe the class of picolinamide antibacterials which show potent and selective activity against C. difficile. The structure-activity relationship of 108 analogues of isonicotinamide 4, a compound that is equally active against methicillin-resistant Staphylococcus aureus and C. difficile, was investigated. Introduction of the picolinamide core as exemplified by analogue 87 resulted in exquisite potency and selectivity against C. difficile. The ability of the picolinamide class to selectively target C. difficile and to prevent gut dysbiosis holds promise for the treatment of recurrent C. difficile infection.
ARYLAMIDE DERIVATIVES AS TTX-S BLOCKERS
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Page/Page column 116-117, (2012/05/05)
The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
Cyanophenyl derivative
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Page column 19, (2010/11/30)
This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.
CYANOPHENYL DERIVATIVES
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, (2008/06/13)
This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.
